Methicillin-resistant Staphylococcus aureus (MRSA) is an S. aureus strain that has developed resistance against ß-lactam antibiotics, resulting in a scarcity of a potent cure for treating Staphylococcus infections. In this study, the anti-MRSA and antioxidant activity of the Indonesian mangrove species Sonneratia caseolaris, Avicennia marina, Rhizophora mucronata, and Rhizophora apiculata were studied. Disk diffusion, DPPH, a brine shrimp lethality test, and total phenolic and flavonoid assays were conducted. Results showed that among the tested mangroves, ethanol solvent-based S. caseolaris leaves extract had the highest antioxidant and anti-MRSA activities. An antioxidant activity assay showed comparable activity when compared to ascorbic acid, with an IC50 value of 4.2499 ± 3.0506 ppm and 5.2456 ± 0.5937 ppm, respectively, classifying the extract as a super-antioxidant. Moreover, S. caseolaris leaves extract showed the highest content of strongly associated antioxidative and antibacterial polyphenols, with 12.4% consisting of nontoxic flavonoids with the minimum inhibitory concentration of the ethanol-based S. caseolaris leaves extract being approximately 5000 ppm. LC-MS/MS results showed that phenolic compounds such as azelaic acid and aspirin were found, as well as flavonoid glucosides such as isovitexin and quercitrin. This strongly suggested that these compounds greatly contributed to antibacterial and antioxidant activity. Further research is needed to elucidate the interaction of the main compounds in S. caseolaris leaves extract in order to confirm their potential either as single or two or more compounds that synergistically function as a nontoxic antioxidant and antibacterial against MRSA.
Antibiotic resistance (AR) remains one of the leading global health challenges, mostly implicated in disease-related deaths. The Enterobacteriaceae-producing metallo-β-lactamases (MBLs) are critically involved in AR pathogenesis through Zn-dependent catalytic destruction of β-lactam antibiotics, yet with limited successful clinical inhibitors. The efficacy of relevant broad-spectrum β-lactams including imipenem and meropenem are seriously challenged by their susceptibility to the Zn-dependent carbapenemase hydrolysis, as such, searching for alternatives remains imperative. In this study, computational molecular modelling and virtual screening methods were extensively applied to identify new putative Zn-sensitive broad-spectrum inhibitors of MBLs, specifically imipenemase-1 (IMP-1) from the IBScreen database. Three ligands, STOCK3S-30154, STOCK3S-30418 and STOCK3S-30514 selectively displayed stronger binding interactions with the enzymes compared to reference inhibitors, imipenem and meropenem. For instance, the ligands showed molecular docking scores of -9.450, -8.005 and -10.159 kcal/mol, and MM-GBSA values of -40.404, -31.902 and -33.680 kcal/mol respectively against the IMP-1. Whereas, imipenem and meropenem showed docking scores of -9.038 and -10.875 kcal/mol, and MM-GBSA of -31.184 and -32.330 kcal/mol respectively against the enzyme. The ligands demonstrated good thermodynamic stability and compactness in complexes with IMP-1 throughout the 100 ns molecular dynamics (MD) trajectories. Interestingly, their binding affinities and stabilities were significantly affected in contacts with the remodelled Zn-deficient IMP-1, indicating sensitivity to the carbapenemase active Zn site, however, with non-β-lactam scaffolds, tenable to resist catalytic hydrolysis. They displayed ideal drug-like ADMET properties, thus, representing putative Zn-sensitive non-β-lactam inhibitors of IMP-1 amenable for further experimental studies.
A novel series of 5-(3-Chlorophenyl)-2-((N-(substituted)-2-acetamoyl)sulfanyl)-1,3,4-oxadiazole derivatives was efficiently synthesized and screened for antibacterial, hemolytic and thrombolytic activities. The molecule 7c remained the best inhibitor of all selected bacterial strains and furthermore possessed very low toxicity, 8.52±0.31. Compound 7a 7b and 7f showed very good thrombolytic activity relative to Streptokinase employed as reference drug. In addition to low toxicity and moderately good thrombolytic activity, the synthesized compounds possessed excellent to moderate antibacterial activity, relative to ciprofloxacin. All compounds especially 7b and 7f can be consider for further clinical studies and might be helpful in synthesis of new drugs for treatment of cardiovascular diseases.
Cellulosic fiber (CF) in nanoform is emergingly finding its way for COVID-19 solution for instance via nanocomposite/nanoparticle from various abundant biopolymeric waste materials, which may not be widely commercialized when the pandemic strikes recently. The possibility is wide open but needs proper collection of knowledge and research data. Thus, this article firstly reviews CF produced from various lignocellulosic or biomass feedstocks' pretreatment methods in various nanoforms or nanocomposites, also serving together with metal oxide (MeO) antimicrobial agents having certain analytical reporting. CF-MeO hybrid product can be a great option for COVID-19 antimicrobial resistant environment to be proposed considering the long-established CF and MeO laboratory investigations. Secondly, a preliminary pH investigation of 7 to 12 on zinc oxide synthesis discussing on Fouriertransform infrared spectroscopy (FTIR) functional groups and scanning electron microscope (SEM) images are also presented, justifying the knowledge requirement for future stable nanocomposite formulation. In addition to that, recent precursors suitable for zinc oxide nanoparticle synthesis with emergingly prediction to serve as COVID-19 purposes via different products, aligning with CFs or nanocellulose for industrial applications are also reviewed.
In this study, the essential oils of Orthosiphon stamineus Benth and Ficus deltoidea Jack were evaluated for their antibacterial activity against invasive oral pathogens, namely Enterococcus faecalis, Streptococcus mutans, Streptococcus mitis, Streptococcus salivarius, Aggregatibacter actinomycetemcomitans, Porphyromonas gingivalis and Fusobacterium nucleatum. Chemical composition of the oils was analyzed using gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). The antibacterial activity of the oils and their major constituents were investigated using the broth microdilution method (minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC)). Susceptibility test, anti-adhesion, anti-biofilm, checkerboard and time-kill assays were also carried out. Physiological changes of the bacterial cells after exposure to the oils were observed under the field emission scanning electron microscope (FESEM). O. stamineus and F. deltoidea oils mainly consisted of sesquiterpenoids (44.6% and 60.9%, respectively), and β-caryophyllene was the most abundant compound in both oils (26.3% and 36.3%, respectively). Other compounds present in O. stamineus were α-humulene (5.1%) and eugenol (8.1%), while α-humulene (5.5%) and germacrene D (7.7%) were dominant in F. deltoidea. The oils of both plants showed moderate to strong inhibition against all tested bacteria with MIC and MBC values ranging 0.63-2.5 mg/mL. However, none showed any inhibition on monospecies biofilms. The time-kill assay showed that combination of both oils with amoxicillin at concentrations of 1× and 2× MIC values demonstrated additive antibacterial effect. The FESEM study showed that both oils produced significant alterations on the cells of Gram-negative bacteria as they became pleomorphic and lysed. In conclusion, the study indicated that the oils of O. stamineus and F. deltoidea possessed moderate to strong antibacterial properties against the seven strains pathogenic oral bacteria and may have caused disturbances of membrane structure or cell wall of the bacteria.
Synthesis of ZnO-Ag heterostructure nanoparticles was carried out by a precipitation method with cellulose nanocrystals (CNCs) as a stabilizer for antimicrobial and thermal studies. ZnO-Ag nanoparticles were obtained from various weight percentages of added AgNO₃ relative to Zn precursors for evaluating the best composition with enhanced functional properties. The ZnO-Ag/CNCs samples were characterized systematically by TEM, XRD, UV, TGA and DTG. From the TEM studies we observed that ZnO-Ag heterostructure nanoparticles have spherical shapes with size diameters in a 9-35 nm range. The antibacterial activities of samples were assessed against the bacterial species Salmonella choleraesuis and Staphylococcus aureus. The CNC-stabilized ZnO-Ag exhibited greater bactericidal activity compared to cellulose-free ZnO-Ag heterostructure nanoparticles of the same particle size. The incorporation of ZnO-Ag hetreostructure nanoparticles significantly increased the thermal stability of cellulose nanocrystals.
This paper describes the fabrication and characterization of bio-nanocomposite hydrogel beads based on Kappa-Carrageenan (κ-Carrageenan) and bio-synthesized silver nanoparticles (Ag-NPs). The silver nanoparticles were prepared in aqueous Citrullus colocynthis seed extract as both reducing and capping agent. Cross-linked κ-Carrageenan/Ag-NPs hydrogel beads were prepared using potassium chloride as the cross-linker. The hydrogel beads were characterized using XRD and FESEM. Moreover, swelling property of the hydrogel beads was investigated. The Ag release profile of the hydrogels was obtained by fitting the experimental data to power law equation. The direct visualization of the green synthesized Ag-NPs using TEM shows particle size in the range of 23±2nm. The bio-nanocomposite hydrogels showed lesser swelling behavior in comparison with pure κ-Carrageenan hydrogel. Regardless the slow Ag release, κ-Carrageenan/Ag-NPs presented good antibacterial activities against Staphylococcus aureus, Methicilin Resistant Staphylococcus aurous, Peseudomonas aeruginosa and Escherichia coli with maximum zones of inhibition 11±2mm. Cytotoxicity study showed that the bio-nanocomposite hydrogels with non-toxic effect of concentration below 1000μg/mL have great pharmacological potential and a suitable level of safety for use in the biological systems.
In this paper, a green microwave-assisted combustion approach to synthesize ZnO-NPs using zinc nitrate and Citrullus colocynthis (L.) Schrad (fruit, seed and pulp) extracts as bio-fuels is reported. The structure, optical, and colloidal properties of the synthesized ZnO-NP samples were studied. Results illustrate that the morphology and particle size of the ZnO samples are different and depend on the bio-fuel. The XRD results revealed that hexagonal wurtzite ZnO-NPs with mean particle size of 27-85 nm were produced by different bio-fuels. The optical band gap was increased from 3.25 to 3.40 eV with the decreasing of particle size. FTIR results showed some differences in the surface structures of the as-synthesized ZnO-NP samples. This led to differences in the zeta potential, hydrodynamic size, and more significantly, antioxidant activity through scavenging of 1, 1-Diphenyl-2-picrylhydrazyl (DPPH) free radicals. In in vitro cytotoxicity studies on 3T3 cells, a dose dependent toxicity with non-toxic effect of concentration below 0.26 mg/mL was shown for ZnO-NP samples. Furthermore, the as-synthesized ZnO-NPs inhibited the growth of medically significant pathogenic gram-positive (Bacillus subtilis and Methicillin-resistant Staphylococcus aurous) and gram-negative (Peseudomonas aeruginosa and Escherichia coli) bacteria. This study provides a simple, green and efficient approach to produce ZnO nanoparticles for various applications.
A series of novel bionanocomposites were cast using different contents of zinc oxide-silver nanoparticles (ZnO-AgNPs) stabilized by cellulose nanocrystals (CNC) as multifunctional nanosized fillers in poly(vinyl alcohol)/chitosan (PVA/Cs) matrices. The morphological structure, mechanical properties, ultraviolet-visible absorption, and antimicrobial properties of the prepared films were investigated as a function of their CNC/ZnO-AgNP content and compared with PVA/chitosan/CNC bionanocomposite films. X-ray diffraction and field emission scanning electron microscopic analyses showed that the CNC/ZnO-AgNPs were homogeneously dispersed in the PVA/Cs matrix and the crystallinity increased with increasing nanosized filler content. Compared with pure PVA/Cs, the tensile strength and modulus in the films increased from 0.055 to 0.205 GPa and from 0.395 to 1.20 GPa, respectively. Ultraviolet and visible light can be efficiently absorbed by incorporating ZnO-AgNPs into a PVA/Cs matrix, suggesting that these bionanocomposite films show good visibility and ultraviolet-shielding effects. The bionanocomposite films had excellent antimicrobial properties, killing both Gram-negative Salmonella choleraesuis and Gram-positive Staphylococcus aureus. The enhanced physical properties achieved by incorporating CNC/ZnO-AgNPs could be beneficial in various applications.
Commercial low-density polyethylene (LDPE) films were UV/ozone treated and coated using a layer-by-layer (LbL) technique by alternating the deposition of polyethyleneimine (PEI) and poly(acrylic acid) (PAA) polymer solutions and antimicrobial silver (Ag). The effects of the initial pH of the PEI/PAA polymer solutions alternating layers (pH 10.5/4 or 9/6.5) on the antimicrobial activity of the developed LbL coatings combined with Ag against Gram-negative and Gram-positive bacteria were investigated. The results from fourier transform infrared spectroscopy and toluidine blue O assay showed that LDPE LbL coated using PEI/PAA polymer solutions with initial pH of 10.5/4 significantly increased the presence of carboxylic acid groups and after Ag attachment the coating had higher antimicrobial activity against both Gram-negative and Gram-positive bacteria compared to the LDPE LbL coated using PEI/PAA polymer solutions with initial pH of 9/6.5. The LDPE LbL coated films using non-modified pH PEI/PAA polymer solutions decreased the water contact-angle indicating an increased hydrophilicity of the film, also increased the tensile strength and roughness of LDPE LbL coated films compared to uncoated LbL samples. The LDPE LbL coated films attached with Ag(+) were UV/ozone treated for 20 min to oxidise Ag(+) to Ag(0). The presence of Ag(0) (Ag nanoparticles (NPs)) on the LDPE LbL coated films was confirmed by XRD, UV-vis spectrophotometer and colour changes. The overall results demonstrated that the LbL technique has the potential to be used as a coating method containing antimicrobial Ag NPs and that the manufactured films could potentially be applied as antimicrobial packaging.
A biofilm is a community of microorganisms attached to a surface and embedded in a matrix of extracellular polymeric substances. Biofilms confer resistance towards conventional antibiotic treatments; thus, there is an urgent need for newer and more effective antimicrobial agents that can act against these biofilms. Due to this situation, various studies have been done to investigate the anti-biofilm effects of natural products including bioactive compounds extracted from microorganisms such as Actinobacteria. This review provides an insight into the anti-biofilm potential of Actinobacteria against various pathogenic bacteria, which hopefully provides useful information, guidance, and improvements for future antimicrobial studies. Nevertheless, further research on the anti-biofilm mechanisms and compound modifications to produce more potent anti-biofilm effects are required.
Over the last few years, several attempts have been made to replace petrochemical products with renewable and biodegradable components. The most challenging part of this approach is to obtain bio-based materials with properties and functions equivalent to those of synthetic products. Various naturally occurring polymers such as starch, collagen, alginate, cellulose, and chitin represent attractive candidates as they could reduce dependence on synthetic products and consequently positively impact the environment. Chitosan is also a unique bio-based polymer with excellent intrinsic properties. It is known for its anti-bacterial and film-forming properties, has high mechanical strength and good thermal stability. Nanotechnology has also applied chitosan-based materials in its most recent achievements. Therefore, numerous chitosan-based bionanocomposites with improved physical and chemical characteristics have been developed in an eco-friendly and cost-effective approach. This review discusses various sources of chitosan, its properties and methods of modification. Also, this work focuses on diverse preparation techniques of chitosan-based bionanocomposites and their emerging application in various sectors. Additionally, this review sheds light on future research scope with some drawbacks and challenges to motivate the researchers for future outstanding research works.
The spread of drug-resistant bacteria has imparted a sense of urgency in the search for new antibiotics. In an effort to develop a new generation of antibacterial agents, we have designed de novo charged lipopeptides inspired by natural antimicrobial peptides. These short lipopeptides are composed of cationic lysine and hydrophobic lipoamino acids that replicate the amphiphilic properties of natural antimicrobial peptides. The resultant lipopeptides were found to self-assemble into nanoparticles. Some were effective against a variety of Gram-positive bacteria, including strains resistant to methicillin, daptomycin and/or vancomycin. The lipopeptides were not toxic to human kidney and liver cell lines and were highly resistant to tryptic degradation. Transmission electron microscopy analysis of bacteria cells treated with lipopeptide showed membrane-damage and lysis with extrusion of cytosolic contents. With such properties in mind, these lipopeptides have the potential to be developed as new antibacterial agents against drug-resistant Gram-positive bacteria.
Natural clays have recently been proven to possess antibacterial properties. Effective natural antimicrobial agents are needed to combat bacterial contamination on food contact surfaces, which are increasingly more prevalent in the food chain. This study sought to determine the antibacterial activity of clays against the food-borne pathogens Salmonella typhimurium ATCC 14028 and Staphylococcus aureus ATCC 13565. Soils were processed to yield leachates and suspensions from untreated and treated clays. Soil particle size, pH, cation-exchange capacity, metal composition and mineralogy were characterized. Antibacterial screening was performed on six Malaysian soils via the disc diffusion method. In addition, a time-kill assay was conducted on selected antibacterial clays after 6 h of exposure. The screening revealed that Munchong and Carey clays significantly inhibit Salmonella typhimurium (11.00 ± 0.71 mm) and S. aureus (7.63 ± 0.48 mm), respectively. Treated Carey clay leachate and suspension completely kill Salmonella typhimurium, while S. aureus viability is reduced (2 to 3 log10). The untreated Carey and all Munchong clays proved ineffective as antibacterials. XRD analysis confirmed the presence of pyrite and magnetite. Treated Carey clays had a higher soluble metal content compared to Munchong; namely Al (92.63 ± 2.18 mg/L), Fe (65.69 ± 3.09 mg/L) and Mg (88.48 ± 2.29 mg/L). Our results suggest that metal ion toxicity is responsible for the antibacterial activity of these clays.
Skin and soft tissue infections are major concerns with respect to wound repair. Recently, anti-bacterial wound dressings have been emerging as promising candidates to reduce infection, thus accelerating the wound healing process. This paper presents our work to develop and characterize poly(vinyl alcohol) (PVA)/chitosan (CS)/silk sericin (SS)/tetracycline (TCN) porous nanofibers, with diameters varying from 305 to 425 nm, both in vitro and in vivo for potential applications as wound dressings. The fabricated nanofibers possess a considerable capacity to take up water through swelling (~325-650%). Sericin addition leads to increased hydrophilicity and elongation at break while decreasing fiber diameter and mechanical strength. Moreover, fibroblasts (L929) cultured on the nanofibers with low sericin content (PVA/CS/1-2SS) displayed greater proliferation compared to those on nanofibers without sericin (PVA/CS). Nanofibers loaded with high sericin and tetracycline content significantly inhibited the growth of Escherichia coli and Staphylococcus aureus. In vivo examination revealed that PVA/CS/2SS-TCN nanofibers enhance wound healing, re-epithelialization, and collagen deposition compared to traditional gauze and nanofibers without sericin. The results of this study demonstrate that the PVA/CS/2SS-TCN nanofiber creates a promising alternative to traditional wound dressing materials.
Recently, the phyco-synthesis of nanoparticles has been applied as a reliable approach to modern research field, and it has yielded a wide spectrum of diverse uses in fields such as biological science and environmental science. This study used marine natural resource seaweed Sargassum myriocystum due to their unique phytochemicals and their significant attributes in giving effective response on various biomedical applications. The response is created by their stress-tolerant environmental adaptations. This inspired us to make an attempt using the above-mentioned charactersitics. Therfore, the current study performed phycosynthesis of titanium dioxide nanoparticles (TiO2-NPs) utilising aqueous extracts of S. myriocystum. The TiO2-NPs formation was confirmed in earlier UV-visible spectroscopy analysis. The crystalline structure, functional groups (phycomolecules), particle morphology (cubic, square, and spherical), size (∼50-90 nm), and surface charge (negative) of the TiO2-NPs were analysed and confirmed by various characterisation analyses. In addition, the seaweed-mediated TiO2-NPs was investigated, which showed potential impacts on antibacterial activity and anti-biofilm actions against pathogens (Staphylococcus aureus, S. epidermidis, Escherichia coli, Proteus vulgaris, Pseudomonas aeruginosa, and Klebsiella pneumoniae). Additionally, some evaluations were performed on larvicidal activities of TiO2-NPs in oppose to Aedes aegypti and Culex quinquefasciatus mosquitos and the environmental effects of photocatalytic activities against methylene blue and crystal violet under sunlight irradiation. The highest percent of methylene blue degradation was observed at 92.92% within 45 min. Overall, our findings suggested that S. myriocystum mediates TiO2-NPs to be a potent disruptive material for bacterial pathogens and mosquito larvae and also to enhance the photocatalytic dye degradation.
Salivaricin B is a 25 amino acid polycyclic peptide belonging to the type AII lantibiotics and first shown to be produced by Streptococcus salivarius. In this study we describe the bactericidal mode of action of salivaricin B against susceptible Gram-positive bacteria. The killing action of salivaricin B required micro-molar concentrations of lantibiotic whereas the prototype lantibiotic nisin A was shown to be potent at nano-molar levels. Unlike nisin A, salivaricin B did not induce pore formation or dissipate the membrane potential in susceptible cells. This was established by measuring the fluorescence of the tryptophan residue at position 17 when salivaricin B interacted with bacterial membrane vesicles. The absence of a fluorescence blue shift indicates a failure of salivaricin B to penetrate the membranes. On the other hand, salivaricin B interfered with cell wall biosynthesis, as shown by the accumulation of the final soluble cell wall precursor UDP-MurNAc-pentapeptide which is the backbone of the bacterial peptidoglycan. Transmission electron microscopy of salivaricin B-treated cells showed a reduction in cell wall thickness together with signs of aberrant septum formation in the absence of visible changes to cytoplasmic membrane integrity.
The leaf extract of a medicinally important plant, watercress (Nasturtium officinale), was obtained through an ultrasound-facilitated method and utilized for the preparation of ZnO nanoparticles via a joint ultrasound-microwave assisted procedure. The characteristics of the extract enriched nanoparticles (Ext/ZnO) were determined by SEM, TEM, XRD, EDX, BET, FTIR, TGA, and UV-Vis DRS analyses and compared to that of ZnO prepared in the absence of the extract (ZnO). The presence of carbon and carbonaceous bonds, changes in the morphology, size, band gap energy, and weight-decay percentage were a number of differences between ZnO and Ext/ZnO that confirmed the link of extract over nanoparticles. Ext/ZnO, watercress leaf extract, ZnO, and insulin therapies were administrated to treat alloxan-diabetic Wister rats and their healing effectiveness results were compared to one another. The serum levels of the main diabetic indices such as insulin, fasting blood glucose, and lipid profile (total triglyceride, total cholesterol, and high-density lipoprotein cholesterol) were estimated for healthy, diabetic, and the rats rehabilitated with the studied therapeutic agents. The watercress extract-enriched ZnO nanoparticles offered the best performance and suppressed the diabetic status of rats. Moreover, both ZnO samples satisfactory inhibited the activities of Staphylococcus aureus and Escherichia coli bacteria. Based on the results, the application of Nasturtium officinale leaf extract can strongly empower ZnO nanoparticles towards superior antidiabetic and enhanced antibacterial activities.
The synthesis of nanoparticles often result in the generation of harmful chemical pollutants. As such, many researchers have focused on developing green processes, which include the biosynthesis. In this research, ZnO nanoparticles were prepared using the leaf extract of whortleberry (Vaccinium arctostaphylos L.) via a simple ultrasonic-assisted method. The morphology, crystal size and structure, surface, thermal, and optical properties of the bio-mediated ZnO sample (ZnOext) were analyzed and compared with that produced without incorporating the extract (ZnOchem). The ZnO samples were evaluated for their antidiabetic, antibacterial, as well as their sono- and photo-catalytic performances. Initially, the samples were intraperitoneal injected to alloxan-diabetic rats to examine their treatment efficiency in terms of effects on fasting blood glucose, insulin, cholesterol, high-density lipoprotein, and total triglyceride levels. The ZnOext showed significantly higher efficiency for improving the health status of alloxan-diabetic rats in contrast with other tested treatments, vis. ZnOchem, insulin, and only leaf extract. In addition, both the ZnO samples were assessed against gram-negative and gram-positive bacteria and through sono- and photo-catalytic processes for removing rhodamine B, respectively. The results of this study indicated that not only the ZnOext sample was pollution free, it also exhibited higher potentials for treating diabetic rats, bacterial decontamination, and also oxidative removal of organic compounds under the influences of ultrasound and UV irradiations when compared with ZnOchem sample.
A facile stereoselective synthesis of novel dispiro indeno pyrrolidine/pyrrolothiazole-thiochroman hybrids has been achieved by 1,3-dipolar cycloaddition of azomethine ylides, generated in situ from ninhydrin and sarcosine/thiaproline, on a series of 3-benzylidenethiochroman-4-ones. The synthesised compounds were screened for their antimycobacterial, anticancer and AchE inhibition activities. Compound 4l (IC50 1.07μM) has been found to exhibit the most potent antimycobacterial activity compared to cycloserine (12 times), pyrimethamine (37 times) and ethambutol (IC50 <1.56μM) and 6l (IC50=2.87μM) is more active than both cycloserine (4 times) and pyrimethamine (12 times). Three compounds, 4a, 6b and 6i, display good anticancer activity against CCRF-CEM cell lines. Compounds 6g and 4g display maximum AchE inhibitory activity with IC50 values of 1.10 and 1.16μmol/L respectively.